Lovastatin



Better Known as: Mevacor

 * Marketed By: Merck & Co.


 * Major Indication: Hyperlipidemia & High Cholesterol (Hypercholesterolemia)


 * Drug Class: HMGR Inhibitor or Statin
 * Date of FDA Approval (Patent Expiration): 1991 (2001)


 * 2000 Sales: $520 Million
 * Importance: Was the first HMG-CoA Inhibitor. Statins are so ubiquitous, doctors have even suggested handing them out with fast food. See: the article


 * See Pharmaceutical Drugs for more information about other drugs and disorders

Mechanism of Action
Lovastatin is rapidly hydrolyzed in vivo into its corresponding b-hydroxyacid, which is an inhibitor of HMG-CoA Reductase (HMGR), a highly regulated enzyme responsible for the committed step in cholesterol synthesis. Lovastatin outcompetes HMG-CoA, the substrate of HMGR, in binding to HMGR.